醋酸炔诺酮单根皮下埋植剂植入后女性体内醋酸炔诺酮的药代动力学

Pharmacokinetics of norethindrone acetate in women after the insertion of a single subdermal implant releasing norethindrone acetate.

作者信息

Singh H, Uniyal J P, Jha P, Takker D, Murguesan K, Hingorani V, Laumas K R

出版信息

Acta Endocrinol (Copenh). 1982 Feb;99(2):302-8. doi: 10.1530/acta.0.0990302.

DOI:10.1530/acta.0.0990302

Abstract

The metabolic clearance rate (MCR) of norethindrone acetate (NETA) and norethindrone (NET) levels in plasma were studied after an iv injection of [3H]NETA in three women before and at 1 week, 1, 2 and 6 months following the insertion of a single silastic subdermal implant releasing microquantities of NETA. No significant change in the MCR of NETA was observed at 1 week (459 +/- 72 1/day), 1 month (489 +/- 113 1/day) and 2 months (522 +/- 144 1/day) compared with that of control (525 +/- 108 1/day). However, MCR of NETA showed significant increase in women exposed to continuous presence of NETA for a period of 6 months (608 +/- 121 1/day; P less than 0.025). NETA was rapidly and extensively metabolized into NET. At 1 week, 1, 2 and 6 months of study, NET was observed to be present in higher amounts compared with NETA. The production rate (PR) of progesterone decreased significantly at 2 and 6 months of NETA implant insertion compared with the PR before the insertion of implant.

摘要

在三名女性静脉注射[3H]醋酸炔诺酮（NETA）后，研究了单根释放微量NETA的硅橡胶皮下植入物植入前及植入后1周、1个月、2个月和6个月时血浆中醋酸炔诺酮（NETA）和炔诺酮（NET）水平的代谢清除率（MCR）。与对照组（525±108 l/天）相比，NETA的MCR在1周（459±72 l/天）、1个月（489±113 l/天）和2个月（522±144 l/天）时未观察到显著变化。然而，在持续接触NETA 6个月的女性中，NETA的MCR显著增加（608±121 l/天；P＜0.025）。NETA迅速且广泛地代谢为NET。在研究的1周、1个月、2个月和6个月时，观察到NET的含量高于NETA。与植入前相比，植入NETA后2个月和6个月时孕酮的生成率（PR）显著降低。